3-Hydroxy-1,5-dihydro-2H-pyrrol-2-ones as novel antibacterial scaffolds against methicillin-resistant Staphylococcus aureus

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

卷:28

Article

Cusumano, Alexander Q.¹  Pierce, Joshua G.^1,2 

[1] NC State Univ, Dept Chem, Coll Sci, Raleigh, NC 27695 USA

[2] NC State Univ, Comparat Med Inst, Raleigh, NC 27695 USA

关键词: Natural products;    Antibiotics;    Heterocycles;    Cyclization;    Medicinal chemistry;   

DOI  :  10.1016/j.bmcl.2018.02.047

来源: Elsevier

【 摘 要 】

Herein, we report the synthesis and evaluation of 3-hydroxy-1,5-dihydro-2H-pyrrol-2-ones as antibacterial agents against methicillin-resistant S. aureus (MRSA) and methicillin-resistant S. epidermidis (MRSE). Lead compound 38 showed minimum inhibitory concentrations (MICs) of 8 and 4 mu g/mL against MRSA and MRSE, respectively. Furthermore, compound 38 displayed a MIC of 8-16 mu g/mL against linezolid-resistant MRSA. These molecules, previously underexplored as antibacterial agents, serve as a new scaffold for antimicrobial development. (C) 2018 Elsevier Ltd. All rights reserved.

【 授权许可】

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